CA2412181A1 - Dipeptide inhibitors for the blood-clotting factor xa - Google Patents

Dipeptide inhibitors for the blood-clotting factor xa Download PDF

Info

Publication number: CA2412181A1
Authority: CA; Canada
Prior art keywords: residue; inhibitors; branched; atoms; substituted
Prior art date: 2000-06-15
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Abandoned

Application number

CA002412181A

Other languages

English (en)

French (fr)

Inventor

Jorg Sturzebecher

Torsten Steinmetzer

Sebastian Kunzel

Andrea Schweinitz

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Curacyte AG

Original Assignee

Individual

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2000-06-15

Filing date

2001-06-15

Publication date

2002-12-09

2001-06-15 Application filed by Individual filed Critical Individual

2002-12-09 Publication of CA2412181A1 publication Critical patent/CA2412181A1/en

Status Abandoned legal-status Critical Current

Links

239000003112 inhibitor Substances 0.000 title claims abstract description 24
108010074860 Factor Xa Proteins 0.000 title claims description 10
108010016626 Dipeptides Proteins 0.000 title 1
239000003114 blood coagulation factor Substances 0.000 title 1
150000001413 amino acids Chemical class 0.000 claims abstract description 8
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125000003118 aryl group Chemical group 0.000 claims description 5
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125000000217 alkyl group Chemical group 0.000 claims 6
125000004432 carbon atom Chemical group C* 0.000 claims 6
125000003710 aryl alkyl group Chemical group 0.000 claims 3
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125000001072 heteroaryl group Chemical group 0.000 claims 3
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125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 2
DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical group C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims 1
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
- C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
- C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
- C07K5/06069—Ser-amino acid
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06086—Dipeptides with the first amino acid being basic

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Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Molecular Biology (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Biochemistry (AREA)
Public Health (AREA)
Bioinformatics & Cheminformatics (AREA)
General Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
Engineering & Computer Science (AREA)
Chemical Kinetics & Catalysis (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Hematology (AREA)
Diabetes (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Peptides Or Proteins (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Superconductors And Manufacturing Methods Therefor (AREA)
Glass Compositions (AREA)
External Artificial Organs (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

CA002412181A 2000-06-15 2001-06-15 Dipeptide inhibitors for the blood-clotting factor xa Abandoned CA2412181A1 (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
DE10029015.9		2000-06-15
DE10029015A DE10029015A1 (de)	2000-06-15	2000-06-15	Hemmstoffe für den Gerinnungsfaktor Xa
PCT/EP2001/006814 WO2001096366A2 (de)	2000-06-15	2001-06-15	Dipeptidische hemmstoffe für den gerinnungsfaktor xa

Publications (1)

Publication Number	Publication Date
CA2412181A1 true CA2412181A1 (en)	2002-12-09

Family

ID=7645522

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CA002412181A Abandoned CA2412181A1 (en)	2000-06-15	2001-06-15	Dipeptide inhibitors for the blood-clotting factor xa

Country Status (8)

Country	Link
US (1)	US6841701B2 (de)
EP (1)	EP1294741B1 (de)
JP (1)	JP2004503563A (de)
AT (1)	ATE289319T1 (de)
AU (2)	AU8184301A (de)
CA (1)	CA2412181A1 (de)
DE (2)	DE10029015A1 (de)
WO (1)	WO2001096366A2 (de)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7838560B2 (en)	2002-03-11	2010-11-23	The Medicines Company (Leipzig) Gmbh	Urokinase inhibitors, production and use thereof
US8124587B2 (en)	2005-09-16	2012-02-28	The Medicines Company (Leipzig) Gmbh	2-(aminomethyl)-5-chlorobenzylamide derivatives and their use as inhibitors of the clotting factor Xa
US8207378B2 (en)	2006-10-24	2012-06-26	The Medicines Company (Leipzig) Gmbh	Trypsin-like serine protease inhibitors, and their preparation and use
US9365613B2 (en)	2003-01-15	2016-06-14	The Medicines Company (Leipzig) Gmbh	Acylated 4-amidino- and -4-guanidinobenzylamines for inhibition of plasma kallikrein

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE60034447T2 (de) *	2000-08-11	2008-02-14	Wilex Ag	Nicht-kovalente Urokinase-und Angiogenese-Inhibitoren
CA2387002A1 (en) *	2000-08-11	2002-02-21	Corvas International, Inc.	Non-covalent inhibitors of urokinase and blood vessel formation
AU2002352245B2 (en) *	2001-12-12	2008-10-16	Wilex Ag	Selective arylguanidine peptides as urokinase inhibitors
DE10210590A1 (de) *	2002-03-11	2003-10-02	Curacyte Ag	Hemmstoffe des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
DE10342108A1 (de) *	2003-09-11	2005-04-14	Curacyte Chemistry Gmbh	Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
AU2006286752B2 (en) *	2005-08-29	2011-10-06	Wilex Ag	Oxadiazole compounds as urokinase inhibitors
KR101503958B1 (ko) *	2007-08-31	2015-03-18	디에스엠 아이피 어셋츠 비.브이.	미용 및/또는 피부과학적 용도의 4-아미디노 벤질아민
EP2590945B1 (de)	2010-07-07	2014-04-30	The Medicines Company (Leipzig) GmbH	Serinproteasehemmer
NO2655399T3 (de)	2010-12-21	2018-02-24

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* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
SE9301916D0 (sv) *	1993-06-03	1993-06-03	Ab Astra	New peptides derivatives
US5707966A (en) *	1994-03-04	1998-01-13	Eli Lilly And Company	Antithrombotic agents
US5705487A (en) *	1994-03-04	1998-01-06	Eli Lilly And Company	Antithrombotic agents
US5726159A (en) *	1994-03-04	1998-03-10	Eli Lilly And Company	Antithrombotic agents
DE69532754T2 (de)	1994-04-26	2005-03-10	Aventis Pharmaceuticals, Inc.	Faktor xa inhibitoren
CZ245797A3 (cs)	1995-02-17	1998-06-17	Basf Aktiengesellschaft	Derivát amidinu dipeptidu jako inhibitor thrombinu
US5914319A (en)	1995-02-27	1999-06-22	Eli Lilly And Company	Antithrombotic agents
US5710130A (en) *	1995-02-27	1998-01-20	Eli Lilly And Company	Antithrombotic agents
FR2791683A1 (fr)	1999-03-30	2000-10-06	Synthelabo	Derives de n-sulfonyl-dipeptides, leur preparation et leur application en therapeutique

2000
- 2000-06-15 DE DE10029015A patent/DE10029015A1/de not_active Withdrawn
2001
- 2001-06-15 US US10/311,364 patent/US6841701B2/en not_active Expired - Lifetime
- 2001-06-15 AT AT01960319T patent/ATE289319T1/de not_active IP Right Cessation
- 2001-06-15 WO PCT/EP2001/006814 patent/WO2001096366A2/de active IP Right Grant
- 2001-06-15 DE DE50105373T patent/DE50105373D1/de not_active Expired - Fee Related
- 2001-06-15 CA CA002412181A patent/CA2412181A1/en not_active Abandoned
- 2001-06-15 AU AU8184301A patent/AU8184301A/xx active Pending
- 2001-06-15 EP EP01960319A patent/EP1294741B1/de not_active Expired - Lifetime
- 2001-06-15 AU AU2001281843A patent/AU2001281843B8/en not_active Ceased
- 2001-06-15 JP JP2002510507A patent/JP2004503563A/ja active Pending

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7838560B2 (en)	2002-03-11	2010-11-23	The Medicines Company (Leipzig) Gmbh	Urokinase inhibitors, production and use thereof
US8476306B2 (en)	2002-03-11	2013-07-02	The Medicines Company (Leipzig) Gmbh	Urokinase inhibitors, production and use thereof
US9365613B2 (en)	2003-01-15	2016-06-14	The Medicines Company (Leipzig) Gmbh	Acylated 4-amidino- and -4-guanidinobenzylamines for inhibition of plasma kallikrein
US8124587B2 (en)	2005-09-16	2012-02-28	The Medicines Company (Leipzig) Gmbh	2-(aminomethyl)-5-chlorobenzylamide derivatives and their use as inhibitors of the clotting factor Xa
US8207378B2 (en)	2006-10-24	2012-06-26	The Medicines Company (Leipzig) Gmbh	Trypsin-like serine protease inhibitors, and their preparation and use
US8410310B2 (en)	2006-10-24	2013-04-02	The Medicines Company (Leipzig) Gmbh	Trypsin-like serine protease inhibitors, and their preparation and use

Also Published As

Publication number	Publication date
AU2001281843B8 (en)	2005-10-06
ATE289319T1 (de)	2005-03-15
EP1294741A2 (de)	2003-03-26
US6841701B2 (en)	2005-01-11
US20030166577A1 (en)	2003-09-04
DE10029015A1 (de)	2001-12-20
JP2004503563A (ja)	2004-02-05
WO2001096366A2 (de)	2001-12-20
AU2001281843B2 (en)	2005-06-09
EP1294741B1 (de)	2005-02-16
AU8184301A (en)	2001-12-24
WO2001096366A3 (de)	2002-04-25
DE50105373D1 (de)	2005-03-24

Publication	Publication Date	Title
CA2338524C (en)	2013-01-22	Inhibitors of urokinase and blood vessel formation
US5858979A (en)	1999-01-12	Inhibitors and substrates of thrombin
US5869454A (en)	1999-02-09	Arginine keto-amide enzyme inhibitors
US5288707A (en)	1994-02-22	Borolysine peptidomimetics
CA2411981C (en)	2010-12-21	Urokinase inhibitors
US6114358A (en)	2000-09-05	Thrombin inhibitors
CA1312702C (en)	1993-01-12	Oligopeptidyl nitrile derivatives, agents containing them, a process for their preparation, and their use
AU2001281843B8 (en)	2005-10-06	Dipeptide inhibitors for the blood-clotting factor Xa
IL99163A (en)	1996-01-19	Peptides comprising c-terminal boronic acid derivatives having serine protease inhibiting activity their preparation and pharmaceutical compositions containing them
US5639739A (en)	1997-06-17	Imidazole containing aminoboronic acids
HU221311B1 (en)	2002-09-28	Perfluoroalkyl tripeptides inhibitors of elastase, pharmaceutical compositions comprising thereof and their use
AU4111700A (en)	2000-11-14	Low-molecular inhibitors of complement proteases
JP4898091B2 (ja)	2012-03-14	ウロキナーゼの阻害剤、それらの製造および使用
JP3623799B2 (ja)	2005-02-23	新しいエラスターゼ阻害剤
JP4942481B2 (ja)	2012-05-30	凝固因子Ｘａ阻害剤として用いるための塩基−置換ベンジルアミン類似体、それらの製法および使用
CA2478412A1 (en)	2003-09-18	Inhibitors of the blood-clotting factor xa, production thereof and use of the same
US20030096759A1 (en)	2003-05-22	Novel elastase inhibitors
JPH11500433A (ja)	1999-01-12	セリンプロテアーゼ阻害剤
US5500414A (en)	1996-03-19	Derivatives of peptides usable as inhibitors of bacterial collagenases
US5648338A (en)	1997-07-15	Inhibitors and substrates of thrombin
WO1994021650A1 (en)	1994-09-29	Boronic acid and ester inhibitors of thrombin
CA1141374A (en)	1983-02-15	Preparation of dehydropeptides
JP2002519430A (ja)	2002-07-02	ヒトアンギオテンシン変換酵素のｎ−末端部位選択的阻害薬

Legal Events

Date	Code	Title	Description
2005-09-12	EEER	Examination request
2008-06-16	FZDE	Discontinued